Assay Detail
Binding
CHEMBL1074647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PARP1 by scintillation proximity assay
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 7.87 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595679 | — | — | 1 | 9.30 |
| CHEMBL595018 | — | — | 1 | 9.00 |
| CHEMBL596354 | — | — | 1 | 9.00 |
| CHEMBL593363 | — | — | 1 | 9.00 |
| CHEMBL593364 | — | — | 1 | 9.00 |
| CHEMBL610165 | — | — | 1 | 8.40 |
| CHEMBL596168 | — | — | 1 | 8.40 |
| CHEMBL596390 | — | — | 1 | 8.40 |
| CHEMBL595236 | — | — | 1 | 8.30 |
| CHEMBL594976 | — | — | 1 | 8.30 |
| CHEMBL595926 | — | — | 1 | 8.30 |
| CHEMBL595019 | — | — | 1 | 8.22 |
| CHEMBL595928 | — | — | 1 | 8.22 |
| CHEMBL611322 | — | — | 1 | 8.22 |
| CHEMBL609002 | — | — | 1 | 8.22 |
| CHEMBL611049 | — | — | 1 | 8.15 |
| CHEMBL594521 | — | — | 1 | 8.15 |
| CHEMBL596389 | — | — | 1 | 8.10 |
| CHEMBL611621 | — | — | 1 | 8.05 |
| CHEMBL595693 | — | — | 1 | 8.05 |
| CHEMBL595680 | — | — | 1 | 8.05 |
| CHEMBL593593 | — | — | 1 | 8.00 |
| CHEMBL593837 | — | — | 1 | 7.96 |
| CHEMBL596391 | — | — | 1 | 7.96 |
| CHEMBL611958 | — | — | 1 | 7.96 |
| CHEMBL595692 | — | — | 1 | 7.92 |
| CHEMBL593592 | — | — | 1 | 7.89 |
| CHEMBL593201 | — | — | 1 | 7.89 |
| CHEMBL592909 | — | — | 1 | 7.89 |
| CHEMBL593202 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595679 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL595018 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL593364 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL596354 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL593363 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL610165 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL596168 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL596390 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL595236 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL594976 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL595926 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL611322 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL609002 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL595928 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL595019 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL611049 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL594521 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL596389 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL611621 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL595693 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL595680 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL593593 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL611958 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL596391 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL593837 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL595692 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL593592 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL593201 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL592909 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL593202 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL593133 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL595694 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL595681 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL594522 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL595927 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL595237 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL603318 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL594999 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL594975 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL594599 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL595464 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL592910 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL608994 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL593611 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL594759 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL594596 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL81977 | 3-AMINOBENZAMIDE | IC50 | = | 3300.0 | nM | 5.48 |